title: Overcoming doxorubicin-resistance in the NCI/ADR-RES model cancer cell line by novel anthracene-9,10-dione derivatives.
abstract: Overcoming drug resistance with remarkable cytotoxic activity by anthracene-9,10-dione derivatives would offer a potential therapeutic strategy. In this study, we report the synthesis and the cytotoxicity of a novel set of anthraquninones. (4-(4-Aminobenzylamino)-9,10-dioxo-9,10-dihydroanthracen-1-yl-4-methylbenzenesulfonate) (3) has excellent in vitro cytotoxicity against doxorubicin-resistant cancer cell line (IC50=0.8 μM), 20-fold higher than doxorubicin. The cytotoxic effect via G2/M arrest does not appear to be ROS.
authors.affiliation: Program of Biotechnology, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
authors.forename: Supranee
authors.initials: S
authors.lastname: Sangthong
authors.forename: Helen
authors.initials: H
authors.lastname: Ha
authors.forename: Thapong
authors.initials: T
authors.lastname: Teerawattananon
authors.forename: Nattaya
authors.initials: N
authors.lastname: Ngamrojanavanich
authors.forename: Nouri
authors.initials: N
authors.lastname: Neamati
authors.forename: Nongnuj
authors.initials: N
authors.lastname: Muangsin
mesh_terms: D000880:Anthraquinones / Q000737:chemistry / Q000494:pharmacology*; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004317:Doxorubicin / Q000494:pharmacology*; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans
chemical_list: D000880:Anthraquinones; D000903:Antibiotics, Antineoplastic; D004317:Doxorubicin
keywords: Anthraquinone derivatives; Cytotoxic mechanism; Doxorubicin-resistance